ECSP099821A - METABOLITES OF THE JANUS QUINASA INHIBITOR (R) -3- (4- (7H-PIRROLO [2,3-d] PIRIMIDIN-4-IL) -1H-PIRAZOL-1-IL) -3-CYCLOPENTILPROPANONITRILE - Google Patents
METABOLITES OF THE JANUS QUINASA INHIBITOR (R) -3- (4- (7H-PIRROLO [2,3-d] PIRIMIDIN-4-IL) -1H-PIRAZOL-1-IL) -3-CYCLOPENTILPROPANONITRILEInfo
- Publication number
- ECSP099821A ECSP099821A EC2009009821A ECSP099821A ECSP099821A EC SP099821 A ECSP099821 A EC SP099821A EC 2009009821 A EC2009009821 A EC 2009009821A EC SP099821 A ECSP099821 A EC SP099821A EC SP099821 A ECSP099821 A EC SP099821A
- Authority
- EC
- Ecuador
- Prior art keywords
- janus
- metabolites
- cyclopentilpropanonitrile
- quinasa
- pirimidin
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Transplantation (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Genetics & Genomics (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Biomedical Technology (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
Abstract
La presente invención provee metabolitos activos de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo que modulan la actividad de Janus quinasas y son útiles para el tratamiento de enfermedades relacionadas con la actividad de Janus quinasas que incluyen, por ejemplo, enfermedades relacionadas con el sistema inmune, trastornos cutáneos, trastornos proliferativos mieloides, cáncer y otras enfermedades.The present invention provides active metabolites of 3- (4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanonitrile that modulate the activity of Janus kinases and they are useful for the treatment of diseases related to the activity of Janus kinases that include, for example, diseases related to the immune system, skin disorders, myeloid proliferative disorders, cancer and other diseases.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US94369507P | 2007-06-13 | 2007-06-13 | |
PCT/US2008/066658 WO2008157207A2 (en) | 2007-06-13 | 2008-06-12 | Metabolites of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-lh-pyrazol-l-yl)-3- cyclopentylpropanenitrile |
Publications (1)
Publication Number | Publication Date |
---|---|
ECSP099821A true ECSP099821A (en) | 2010-01-29 |
Family
ID=40029276
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EC2009009821A ECSP099821A (en) | 2007-06-13 | 2009-12-21 | METABOLITES OF THE JANUS QUINASA INHIBITOR (R) -3- (4- (7H-PIRROLO [2,3-d] PIRIMIDIN-4-IL) -1H-PIRAZOL-1-IL) -3-CYCLOPENTILPROPANONITRILE |
Country Status (26)
Country | Link |
---|---|
US (5) | US7834022B2 (en) |
EP (1) | EP2173751B1 (en) |
JP (1) | JP5479331B2 (en) |
KR (1) | KR20100049008A (en) |
CN (1) | CN101815717B (en) |
AR (1) | AR067024A1 (en) |
AU (1) | AU2008266182B8 (en) |
BR (1) | BRPI0812563A2 (en) |
CA (1) | CA2689158C (en) |
CL (1) | CL2008001709A1 (en) |
CO (1) | CO6251255A2 (en) |
CR (1) | CR11149A (en) |
EA (1) | EA017790B1 (en) |
EC (1) | ECSP099821A (en) |
ES (1) | ES2448868T3 (en) |
GE (1) | GEP20125534B (en) |
HK (1) | HK1141020A1 (en) |
IL (1) | IL202429A0 (en) |
MX (2) | MX2009013403A (en) |
NZ (1) | NZ581801A (en) |
PL (1) | PL2173751T3 (en) |
PT (1) | PT2173751E (en) |
TW (1) | TWI426911B (en) |
UA (1) | UA99465C2 (en) |
WO (1) | WO2008157207A2 (en) |
ZA (1) | ZA200908820B (en) |
Families Citing this family (80)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005105814A1 (en) * | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
LT2426129T (en) | 2005-12-13 | 2017-02-10 | Incyte Holdings Corporation | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors |
WO2008079965A1 (en) | 2006-12-22 | 2008-07-03 | Incyte Corporation | Substituted heterocycles as janus kinase inhibitors |
CL2008001709A1 (en) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compounds derived from pyrrolo [2,3-b] pyrimidine, jak kinase modulators; pharmaceutical composition; and use in the treatment of diseases such as cancer, psoriasis, rheumatoid arthritis, among others. |
RS54878B1 (en) | 2007-06-13 | 2016-10-31 | Incyte Holdings Corp | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
US8309718B2 (en) * | 2007-11-16 | 2012-11-13 | Incyte Corporation | 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors |
KR20130066703A (en) | 2008-02-06 | 2013-06-20 | 노파르티스 아게 | Pyrrolo[2,3-d]pyrimidines and use thereof as tyrosine kinase inhibitors |
JP5275371B2 (en) | 2008-03-11 | 2013-08-28 | インサイト・コーポレイション | Azetidine derivatives and cyclobutane derivatives as JAK inhibitors |
CL2009001884A1 (en) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Use of 3-cyclopentyl-3- [4- (7h-pyrrolo [2,3-d] pyrimidin-4-yl) -1h-pyrazol-1-yl) propanonitrile, janus kinase inhibitor, and use of a composition that understands it for the treatment of dry eye. |
JOP20190231A1 (en) | 2009-01-15 | 2017-06-16 | Incyte Corp | Processes for preparing jak inhibitors and related intermediate compounds |
ES2456275T3 (en) | 2009-02-27 | 2014-04-21 | Ambit Biosciences Corporation | JAK kinase modulator quinazoline derivatives and their use in methods |
UA106078C2 (en) | 2009-05-22 | 2014-07-25 | Інсайт Корпорейшн | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptanenitrile as jak inhibitors |
WO2010135650A1 (en) * | 2009-05-22 | 2010-11-25 | Incyte Corporation | N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS |
WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
JP2011083279A (en) * | 2009-09-16 | 2011-04-28 | Institute Of Physical & Chemical Research | Diagnostic method for skin inflammation disease |
KR101805936B1 (en) * | 2009-10-09 | 2017-12-07 | 인사이트 홀딩스 코포레이션 | Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
JP5858434B2 (en) | 2010-02-18 | 2016-02-10 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Cyclobutane and methylcyclobutane derivatives as Janus kinase inhibitors |
MX364636B (en) | 2010-03-10 | 2019-05-03 | Incyte Corp | Piperidin-4-yl azetidine derivatives as jak1 inhibitors. |
NZ603446A (en) * | 2010-04-14 | 2014-05-30 | Array Biopharma Inc | 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases |
SI2574168T1 (en) * | 2010-05-21 | 2016-07-29 | Incyte Holdings Corporation | Topical formulation for a jak inhibitor |
AU2011296024B2 (en) | 2010-09-01 | 2015-05-28 | Ambit Biosciences Corporation | Quinazoline compounds and methods of use thereof |
WO2012061537A2 (en) * | 2010-11-02 | 2012-05-10 | The Trustees Of Columbia University In The City Of New York | Methods for treating hair loss disorders |
SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
EP2675451B9 (en) | 2011-02-18 | 2017-07-26 | Novartis Pharma AG | mTOR/JAK INHIBITOR COMBINATION THERAPY |
AU2012273164B2 (en) | 2011-06-20 | 2015-05-28 | Incyte Holdings Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
JP2014521725A (en) | 2011-08-10 | 2014-08-28 | ノバルティス・ファルマ・アクチェンゲゼルシャフト | JAKPI3K / mTOR combination therapy |
TW201313721A (en) | 2011-08-18 | 2013-04-01 | Incyte Corp | Cyclohexyl azetidine derivatives as JAK inhibitors |
UA111854C2 (en) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | METHODS AND INTERMEDIATE COMPOUNDS FOR JAK INHIBITORS |
JP2014528475A (en) * | 2011-10-12 | 2014-10-27 | アレイ バイオファーマ、インコーポレイテッド | 5,7-substituted imidazo [1,2-c] pyrimidine |
US10821111B2 (en) | 2011-11-30 | 2020-11-03 | Emory University | Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections |
CN107898790B (en) | 2011-11-30 | 2024-06-21 | 埃默里大学 | Antiviral JAK inhibitors for the treatment or prevention of retroviral and other viral infections |
AR091079A1 (en) | 2012-05-18 | 2014-12-30 | Incyte Corp | DERIVATIVES OF PIRROLOPIRIMIDINA AND PIRROLOPIRIDINA REPLACED WITH PIPERIDINILCICLOBUTILO AS JAK INHIBITORS |
ES2867048T3 (en) | 2012-06-15 | 2021-10-20 | Concert Pharmaceuticals Inc | Ruxolitinib deuterated derivatives |
WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
WO2014016396A1 (en) | 2012-07-27 | 2014-01-30 | Ratiopharm Gmbh | Oral dosage forms for modified release comprising ruxolitinib |
AR093308A1 (en) | 2012-11-01 | 2015-05-27 | Incyte Corp | THYMPHENE FUSIONATED TRICICLIC DERIVATIVES AS JAK INHIBITORS |
JP2015537030A (en) | 2012-11-15 | 2015-12-24 | インサイト・コーポレイションIncyte Corporation | Sustained release dosage form of ruxolitinib |
KR102366356B1 (en) | 2013-03-06 | 2022-02-23 | 인사이트 홀딩스 코포레이션 | Processes and intermediates for making a jak inhibitor |
EA036448B1 (en) | 2013-05-17 | 2020-11-11 | Инсайт Корпорейшн | Bipyrazole derivatives as jak inhibitors |
EP3721873A1 (en) | 2013-08-07 | 2020-10-14 | Incyte Corporation | Sustained release dosage forms for a jak1 inhibitor |
EA201690421A1 (en) | 2013-08-20 | 2016-06-30 | Инсайт Корпорейшн | POSITIVE EFFECT IN THE FORM OF INCREASING THE DURATION OF LIFE IN PATIENTS WITH SALTED TUMORS WITH INCREASED C-REACTIVE PROTEIN LEVELS |
CN111494386A (en) | 2014-04-08 | 2020-08-07 | 因赛特公司 | Treatment of B cell malignancies by combination of JAK and PI3K inhibitors |
BR112016025427A2 (en) | 2014-04-30 | 2017-08-15 | Incyte Corp | processes for preparing a jak1 inhibitor and forms thereof |
WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
CN105218548A (en) * | 2014-06-09 | 2016-01-06 | 上海海和药物研究开发有限公司 | A kind of novel heterocyclic compounds and preparation method thereof and the purposes as kinase inhibitor |
ES2921875T3 (en) | 2014-08-11 | 2022-09-01 | Acerta Pharma Bv | Therapeutic combinations of a BTK inhibitor, a PD-1 inhibitor and/or a PD-L1 inhibitor |
SI3179991T1 (en) | 2014-08-11 | 2022-04-29 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor and a bcl-2 inhibitor |
WO2016024232A1 (en) | 2014-08-11 | 2016-02-18 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor |
WO2017144995A1 (en) | 2016-02-24 | 2017-08-31 | Pfizer Inc. | Pyrazolo[1,5-a]pyrazin-4-yl derivatives as jak-inhibitors |
WO2017192905A1 (en) | 2016-05-04 | 2017-11-09 | Concert Pharmaceuticals, Inc. | Treatment of hair loss disorders with deuterated jak inhibitors |
CN107513067A (en) | 2016-06-16 | 2017-12-26 | 北京赛林泰医药技术有限公司 | Pyrrolopyrimidine compounds containing substituted cyclopenta |
WO2018041989A1 (en) | 2016-09-02 | 2018-03-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating refractory celiac disease type 2 |
TW201924683A (en) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | Low dose combination therapy for treatment of myeloproliferative neoplasms |
AR114810A1 (en) | 2018-01-30 | 2020-10-21 | Incyte Corp | PROCESSES AND INTERMEDIATES TO DEVELOP A JAK INHIBITOR |
IL276725B2 (en) | 2018-02-16 | 2024-09-01 | Incyte Corp | JAK1 pathway inhibitors for the treatment of cytokine-related disorders |
CN113768934A (en) | 2018-03-30 | 2021-12-10 | 因赛特公司 | Treatment of hidradenitis suppurativa with JAK inhibitors |
MA52655A (en) | 2018-03-30 | 2021-02-17 | Incyte Corp | BIOMARKERS FOR INFLAMMATORY SKIN DISEASE |
MX2020010815A (en) | 2018-04-13 | 2020-12-11 | Incyte Corp | Biomarkers for graft-versus-host disease. |
CA3224985A1 (en) | 2018-07-31 | 2020-02-06 | Loxo Oncology, Inc. | Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide |
JP7431845B2 (en) | 2018-10-31 | 2024-02-15 | インサイト・コーポレイション | Combination therapy for the treatment of blood disorders |
JP2022515197A (en) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | 7-((3,5-dimethoxyphenyl) amino) quinoxaline derivative as an FGFR inhibitor for treating cancer |
CN113490666A (en) | 2018-12-19 | 2021-10-08 | 奥瑞生物药品公司 | Substituted pyrazolo [1,5-A ] pyridine compounds as inhibitors of FGFR tyrosine kinases |
CA3124088A1 (en) | 2018-12-20 | 2020-06-25 | Incyte Corporation | Imidazopyridazine and imidazopyridine compounds as inhibitors of activin receptor-like kinase-2 |
WO2020188015A1 (en) | 2019-03-21 | 2020-09-24 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
WO2020201362A2 (en) | 2019-04-02 | 2020-10-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
CA3136468A1 (en) * | 2019-04-12 | 2020-10-15 | Primegene (Beijing) Co., Ltd. | Pyrazolopyrazine derived compounds and pharmaceutical compositions used as jak inhibitors |
WO2020212395A1 (en) | 2019-04-16 | 2020-10-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels |
JP2022551649A (en) | 2019-10-10 | 2022-12-12 | インサイト・コーポレイション | Biomarkers for graft-versus-host disease |
WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
KR20220107213A (en) | 2019-11-22 | 2022-08-02 | 인사이트 코포레이션 | Combination therapy comprising an ALK2 inhibitor and a JAK2 inhibitor |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
TW202210471A (en) | 2020-06-02 | 2022-03-16 | 美商英塞特公司 | Processes of preparing a jak1 inhibitor |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
WO2022036030A1 (en) | 2020-08-12 | 2022-02-17 | Concert Pharmaceuticals, Inc. | Process for preparing enantiomerically enriched jak inhibitors |
US11897889B2 (en) | 2020-08-18 | 2024-02-13 | Incyte Corporation | Process and intermediates for preparing a JAK1 inhibitor |
EP4200300A1 (en) | 2020-08-18 | 2023-06-28 | Incyte Corporation | Process and intermediates for preparing a jak inhibitor |
MX2023006542A (en) | 2020-12-08 | 2023-08-25 | Incyte Corp | Jak1 pathway inhibitors for the treatment of vitiligo. |
WO2023288197A1 (en) | 2021-07-12 | 2023-01-19 | Incyte Corporation | Process and intermediates for preparing baricitinib |
WO2023222565A1 (en) | 2022-05-16 | 2023-11-23 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation |
Family Cites Families (83)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3036390A1 (en) | 1980-09-26 | 1982-05-13 | Troponwerke GmbH & Co KG, 5000 Köln | Antiinflammatory intermediate 7H-pyrrolo-(2,3-D)-pyrimidine derivs. - prepd. by dealkylation of 7-phenyl:ethyl derivs. by reaction with hydrochloric, phosphoric or poly:phosphoric acid |
US5521184A (en) * | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
KR19990028709A (en) | 1995-07-05 | 1999-04-15 | 미리암 디. 메코너헤이 | Fungus pyrimidinone |
DK0836605T3 (en) | 1995-07-06 | 2002-05-13 | Novartis Ag | Pyrrolopyrimidines and Methods for their Preparation |
US6232320B1 (en) * | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
BR9910864A (en) | 1998-06-04 | 2002-02-05 | Abbott Lab | Anti-inflammatory compounds for inhibiting cell adhesion |
EP1087970B1 (en) | 1998-06-19 | 2004-04-28 | Pfizer Products Inc. | PYRROLO 2,3-d]PYRIMIDINE COMPOUNDS |
PA8474101A1 (en) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | PYROLEUM [2,3-D] PIRIMIDINE COMPOUNDS |
BR9912938B1 (en) | 1998-08-11 | 2011-06-28 | isoquinoline derivatives, composition comprising them, process for preparation and use thereof. | |
US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
ATE380031T1 (en) | 1999-12-10 | 2007-12-15 | Pfizer Prod Inc | COMPOSITIONS CONTAINING PYRROLO 2,3-D PYRIMIDINE DERIVATIVES |
NZ519121A (en) * | 1999-12-24 | 2004-05-28 | Aventis Pharma Ltd | Azaindoles useful as Syk kinase inhibitors |
GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
US6335342B1 (en) * | 2000-06-19 | 2002-01-01 | Pharmacia & Upjohn S.P.A. | Azaindole derivatives, process for their preparation, and their use as antitumor agents |
ATE465756T1 (en) * | 2000-06-23 | 2010-05-15 | Mitsubishi Tanabe Pharma Corp | ANTITUMOR EFFECT AMPLIFIER |
ES2257410T3 (en) * | 2000-06-26 | 2006-08-01 | Pfizer Products Inc. | PIRROLO COMPOUNDS (2,3-D) PYRIMIDINE AS IMMUNOSUPPRESSING AGENTS. |
NZ522783A (en) | 2000-06-28 | 2004-07-30 | Smithkline Beecham P | Wet milling process for pharmaceuticals with agitator or chamber having nylon with internal lubricant |
GB0100622D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds V111 |
WO2002060492A1 (en) | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd | Methods of inhibiting kinases |
US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
CA2455181C (en) | 2001-08-01 | 2010-04-06 | Merck & Co., Inc. | Benzimidazo[4,5-f]isoquinolinone derivatives |
CN100391958C (en) | 2001-09-19 | 2008-06-04 | 安万特医药股份有限公司 | Chemical compounds |
HU230798B1 (en) | 2001-10-30 | 2018-06-28 | Novartis Ag | Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity |
GT200200234A (en) | 2001-12-06 | 2003-06-27 | NEW CRYSTAL COMPOUNDS | |
TW200403058A (en) * | 2002-04-19 | 2004-03-01 | Bristol Myers Squibb Co | Heterocyclo inhibitors of potassium channel function |
AR037647A1 (en) | 2002-05-29 | 2004-12-01 | Novartis Ag | USED DIARILUREA DERIVATIVES FOR THE TREATMENT OF DEPENDENT DISEASES OF THE PROTEIN KINase |
GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
JP4688498B2 (en) | 2002-11-04 | 2011-05-25 | バーテックス ファーマシューティカルズ インコーポレイテッド | Heteroaryl-pyrimidine derivatives as JAK inhibitors |
AR042052A1 (en) | 2002-11-15 | 2005-06-08 | Vertex Pharma | USEFUL DIAMINOTRIAZOLS AS INHIBITORS OF PROTEINQUINASES |
AU2003276591A1 (en) | 2002-11-26 | 2004-06-18 | Pfizer Products Inc. | Method of treatment of transplant rejection |
UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
US7407962B2 (en) | 2003-02-07 | 2008-08-05 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors or protein kinases |
GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
SE0301372D0 (en) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
SE0301373D0 (en) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
US20050043346A1 (en) | 2003-08-08 | 2005-02-24 | Pharmacia Italia S.P.A. | Pyridylpyrrole derivatives active as kinase inhibitors |
AR045944A1 (en) | 2003-09-24 | 2005-11-16 | Novartis Ag | ISOQUINOLINE DERIVATIVES 1.4-DISPOSED |
MXPA06005882A (en) | 2003-11-25 | 2006-06-27 | Pfizer Prod Inc | Method of treatment of atherosclerosis. |
KR20060096153A (en) | 2003-12-17 | 2006-09-07 | 화이자 프로덕츠 인코포레이티드 | Pyrrolo [2,3-d] pyrimidine compounds for the treatment of transplant rejection |
US20050187389A1 (en) * | 2004-01-13 | 2005-08-25 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
EP2786995A1 (en) | 2004-03-30 | 2014-10-08 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of JAK and other protein kinases |
WO2005105814A1 (en) | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
WO2005105988A2 (en) | 2004-04-28 | 2005-11-10 | Vertex Pharmaceuticals Incorporated | Crystal structure of human jak3 kinase domain complex and binding pockets thereof |
US20090163523A1 (en) | 2004-05-03 | 2009-06-25 | Philip Lake | Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor |
MXPA06013250A (en) | 2004-05-14 | 2007-02-28 | Abbott Lab | Kinase inhibitors as therapeutic agents. |
PE20060426A1 (en) | 2004-06-02 | 2006-06-28 | Schering Corp | TARTARIC ACID DERIVATIVES AS INHIBITORS OF MMPs, ADAMs, TACE AND TNF-alpha |
WO2006013114A1 (en) | 2004-08-06 | 2006-02-09 | Develogen Aktiengesellschaft | Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome |
UY29177A1 (en) | 2004-10-25 | 2006-05-31 | Astex Therapeutics Ltd | SUBSTITUTED DERIVATIVES OF PURINA, PURINONA AND DEAZAPURINA, COMPOSITIONS THAT CONTAIN METHODS FOR THEIR PREPARATION AND ITS USES |
MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
AU2005309019A1 (en) | 2004-11-24 | 2006-06-01 | Novartis Ag | Combinations of JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors |
AR054416A1 (en) | 2004-12-22 | 2007-06-27 | Incyte Corp | PIRROLO [2,3-B] PIRIDIN-4-IL-AMINAS AND PIRROLO [2,3-B] PIRIMIDIN-4-IL-AMINAS AS INHIBITORS OF THE JANUS KINASES. PHARMACEUTICAL COMPOSITIONS. |
ES2320487T3 (en) * | 2005-02-03 | 2009-05-22 | Vertex Pharmaceuticals, Inc. | PIRROLOPIRIMIDINES USEFUL AS PROTEIN QUINASE INHIBITORS. |
EP2354140A1 (en) | 2005-05-20 | 2011-08-10 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
US20070049591A1 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Inhibitors of MAPK/Erk Kinase |
US20070149506A1 (en) | 2005-09-22 | 2007-06-28 | Arvanitis Argyrios G | Azepine inhibitors of Janus kinases |
EP2532667A1 (en) | 2005-09-30 | 2012-12-12 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
US20130137681A1 (en) | 2005-12-13 | 2013-05-30 | Incyte Corporation | HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS |
LT2426129T (en) | 2005-12-13 | 2017-02-10 | Incyte Holdings Corporation | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors |
JP2009521504A (en) | 2005-12-22 | 2009-06-04 | スミスクライン・ビーチャム・コーポレイション | Akt activity inhibitor |
UA95940C2 (en) | 2006-01-17 | 2011-09-26 | Вертекс Фармасьютикалс Інкорпорейтед | Azaindoles useful as inhibitors of janus kinases |
AU2007235487A1 (en) | 2006-04-05 | 2007-10-18 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
WO2008079965A1 (en) | 2006-12-22 | 2008-07-03 | Incyte Corporation | Substituted heterocycles as janus kinase inhibitors |
CL2008001709A1 (en) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compounds derived from pyrrolo [2,3-b] pyrimidine, jak kinase modulators; pharmaceutical composition; and use in the treatment of diseases such as cancer, psoriasis, rheumatoid arthritis, among others. |
RS54878B1 (en) | 2007-06-13 | 2016-10-31 | Incyte Holdings Corp | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
US8309718B2 (en) | 2007-11-16 | 2012-11-13 | Incyte Corporation | 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors |
JP5275371B2 (en) | 2008-03-11 | 2013-08-28 | インサイト・コーポレイション | Azetidine derivatives and cyclobutane derivatives as JAK inhibitors |
CL2009001884A1 (en) | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Use of 3-cyclopentyl-3- [4- (7h-pyrrolo [2,3-d] pyrimidin-4-yl) -1h-pyrazol-1-yl) propanonitrile, janus kinase inhibitor, and use of a composition that understands it for the treatment of dry eye. |
JOP20190231A1 (en) | 2009-01-15 | 2017-06-16 | Incyte Corp | Processes for preparing jak inhibitors and related intermediate compounds |
WO2010135650A1 (en) | 2009-05-22 | 2010-11-25 | Incyte Corporation | N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS |
UA106078C2 (en) | 2009-05-22 | 2014-07-25 | Інсайт Корпорейшн | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptanenitrile as jak inhibitors |
WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
KR101805936B1 (en) | 2009-10-09 | 2017-12-07 | 인사이트 홀딩스 코포레이션 | Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
JP5858434B2 (en) | 2010-02-18 | 2016-02-10 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Cyclobutane and methylcyclobutane derivatives as Janus kinase inhibitors |
MX364636B (en) | 2010-03-10 | 2019-05-03 | Incyte Corp | Piperidin-4-yl azetidine derivatives as jak1 inhibitors. |
SI2574168T1 (en) | 2010-05-21 | 2016-07-29 | Incyte Holdings Corporation | Topical formulation for a jak inhibitor |
SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
EP2675451B9 (en) | 2011-02-18 | 2017-07-26 | Novartis Pharma AG | mTOR/JAK INHIBITOR COMBINATION THERAPY |
AU2012273164B2 (en) | 2011-06-20 | 2015-05-28 | Incyte Holdings Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
JP2014521725A (en) | 2011-08-10 | 2014-08-28 | ノバルティス・ファルマ・アクチェンゲゼルシャフト | JAKPI3K / mTOR combination therapy |
TW201313721A (en) | 2011-08-18 | 2013-04-01 | Incyte Corp | Cyclohexyl azetidine derivatives as JAK inhibitors |
UA111854C2 (en) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | METHODS AND INTERMEDIATE COMPOUNDS FOR JAK INHIBITORS |
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